WO2021007626A1

WO2021007626A1 - Oral medication for treating lipoedema

Info

Publication number: WO2021007626A1
Application number: PCT/BR2019/000026
Authority: WO
Inventors: Daniel Augusto BENITTI; Alexandre CAMPOS MORAES AMATO
Original assignee: Benitti Daniel Augusto; Campos Moraes Amato Alexandre
Priority date: 2019-07-12
Filing date: 2019-08-06
Publication date: 2021-01-21
Also published as: BR102019014449A2

Abstract

This is a product for use in the pharmaceutical sector. The present invention relates to a new and novel medication for treating lipoedema, which is a chronic hereditary fat distribution disorder characterized by an increase in subcutaneous adipose tissue (lipohypertrophy), by means of a formulation that has been shown to be effective in treating the disease, using various components: Citrus sinensis, Curcumin and Piperine, inter alia.

Description

“ORAL MEDICATION TO TREAT LIPEDEMA”

1. The present invention refers to a new and unprecedented drug for the treatment of “Lipedema”, which is a chronic hereditary dysfunction of fat distribution characterized by an increase in subcutaneous adipose tissue (lipohypertrophy), through a formulation that has been shown to be efficient in the treatment of the disease, using several components: Citrus sinensis, Curcumin, Piperina, among others.

2. The present invention aims to offer an appropriate treatment to people who develop Lipedema, through a remedy and a treatment that also consists of a creamy formulation, to be treated more specifically in another application for an invention patent, making unprecedented treatment in the world. Although it is a common disease that affects 11% of women, it is rarely diagnosed and, when diagnosed, there is no treatment available on the market.

3. It is an oral medication that associated with a topical medication relieves the symptoms of the disease and helps with weight loss avoiding surgery and psychological complications of the patient's evolution. There is no drug treatment for the disease. Surgical only. Therefore, it opens a possibility of treatment for a large population that suffers from severe symptoms and loss of quality of life. We carried out a scientific survey and in the literature the only effective treatment option for the disease is surgical with improvement in the treatment of symptoms in 58% after 6 (six) months (Rapprich et al) and in our scientifically measured experience in a pilot project, we have 34.7% in symptoms with only 1 month of treatment. 4. The medicine is composed of: dry extract of cataloupe melon; Pyrroloquinoline Quinona; Citrus sinensis; Curcumin; Piperine; Lutein, Astaxanthin; Selenium chelate; Vitamin C; Quercetin and Bromelain.

5. Cantaloupe melon (Cucumis melo L.) is a bioavailable form of superoxide dismutase (SOD). SOD reduces oxidative stress by catalyzing the dismutation of superoxide into oxygen and hydrogen peroxide.

6. SOD causes the protection of cognitive function against stress, prevents diseases related to the metabolic syndrome, acts in the prevention of the preclinical stage of atherosclerosis by inhibiting vascular inflammation, decreasing the risk of cardiovascular diseases, decreasing the accumulation of lactic acid during exercise and promotes immune modulation. In the skin, it reduces the signs of aging, helping to maintain the structural integrity of the skin and collagen, in preventing allergies, in preparing the skin for sun exposure, in addition to reducing changes in post-inflammatory and solar hyperpigmentation. (References: Stejnborn, AS; Cloarec, M; Nakajima, S).

7. Pyrroloquinoline Quinone / Neurological and mitochondrial protection Prevention of premature aging.

8. Scientific name: Metoxantin Pyrroloquinoline quinone (PQQ) is a tricyclic quinone that functions as a coenzyme in various bacterial oxide reductase reactions. Also known as methoxyantin, it is considered 100 times more potent than vitamin C, found naturally in foods such as: fermented soybeans, kiwi, parsley, green peppers, spinach, green tea, among others (RUCKER, 2001; TSUGE, 2005) - it is a essential nutrient that the organism cannot synthesize, being a cofactor of oxide-reduction reactions, acting as a powerful antioxidant, with the ability to neutralize free radicals, superoxides and hydroxides, resulting in the reduction of early cell aging, with the consequence of promoting healthy aging. It improves cognitive functions, promotes mitochondrial protection, has antioxidant properties, protects the immune and neurological systems. In addition, studies show that PQQ increases growth factors and contributes to mitochondrial biogenesis (OHWADA, 2008; YAMAGUCHI, 1993). Studies show that PQQ can improve cognitive function, quality of sleep, relief from mental fatigue and positive mood (NAKANO, 2012). Other studies show that PQQ has a positive influence on brain functions, improving memory and attention in healthy elderly people (NAKANO, 2009). By delaying the aging process, it is suggested that PQQ can prevent gray hair - this process is closely linked to the degradation and progressive disappearance of mitochondria and the excess of free radicals in the hair bulb; increases the energy levels indispensable to cells.

9. Properties · Antioxidant · Improves cognitive function. · Neuroprotection · Mitochondrial booster · Increases energy · Improves the immune system · Helps with healthy aging · Cardioprotective action Proving effectiveness.

10. Citrus sinensis is an extract obtained from Moro Vermelha Vermelha, also known as false blood. Moro red orange (Citrus sinensis L.) contains a variety of phytochemical components that contribute to the flavor and properties of the fruit. These substances include sugars like sucrose, fructose and glucose; organic acids (mainly citric, malic and isocitric acid); carotenoids, such as xanthophylls and carotenes; vitamins such as vitamin C, A, B1, B6 and B3; aromatic compounds, including various esters, alcohols, ketones, lactones and volatile hydrocarbons, in addition to polyphenols such as 8-hydroxycinnamic acid and bioflavonoids. Bioflavonoids are composed of several phytochemicals, among which anthocyanins and flavanones stand out, which are present in the species extract in at least 90%. Studies indicate that these assets are responsible for limiting body weight gain, improving insulin sensitivity and decreasing serum triglyceride and total cholesterol levels.

11. Citrus sinensis also has anti-inflammatory, antioxidant and cardioprotective activities.

12. A recent study, published in the prestigious International magazine

Journal of Obesity, showed that the components present in the extract of Moro red orange act synergistically, and reduce the weight gain and the accumulation of fat induced in animals fed a high-fat diet, with a reduction in abdominal fat by 25 to 50%. Histological examination of adipose tissue also showed a marked reduction in the size of adipocytes, due to the decreased ability to accumulate fat.

13. The components of the fruit helped to regulate the production of insulin, a hormone that regulates the synthesis of fat. Suggested associations DM-II ™ also acts in increasing insulin sensitivity, lowering cholesterol, maintaining cardiovascular health and supporting weight reduction, thus its association with

Citrus Sinensis can be beneficial for cholesterol control as well as weight reduction.

14. Curcuma longa is traditionally used for multiple 5

diseases, the rhizomes being the main part of the plant used in the preparations.

15. Rhizomes are mainly used to treat: skin wounds (327-332), flatulence (330, 333, 334), dyspepsia (330, 335, 336), arthritis (327, 337), gastritis (334, 335) , liver disorders (332, 338), jaundice (330, 332), cough (327, 339) and skin diseases (337), such as dermatitis (334, 340), dermatomycosis (341), scabies (330, 342), skin infections (343) and skin parasites (344). In addition, rhizomes are also popularly reported in cases of: diabetes (327), leprosy (344), hirsutism (344), ulcers caused by HPV (344), itchy skin rashes (345), smallpox (328) , chickenpox (328), malaria (346), postpartum bleeding (347), muscle injury (348), asthma (330), worms (342), tonic, revitalizer, stimulant (332, 336), fever, diarrhea, expectorant and anti-inflammatory (334).

16. Piperine (4) is composed of a group 1, 3-benzodioxola (subunit A), next to a chain of pentadiene acid (subunit B) and the fragment piperidine (subunit C). Piperic acid, the acyl portion of the piperine molecule (subunits A and B), has as its precursor the respective cinnamoyl-SCoA derivative (6), which is biosynthesized from shikimic acid (5), and may present different oxygenation patterns in the aromatic ring (in carbons 3, 4 and 5), with the 3,4-methylenedioxy ring being quite common in the class of phenylpropanoids (C6-C3).

17. Lutein is a type of carotenoid and, like all others, is not produced by the human body. It has important functions: it is a natural filter of blue light, which protects the eyes and skin from damage arising in daily life due to exposure to daylight and artificial lighting. environments. It is also a relevant antioxidant that provides protection against oxidative damage from “free radicals” produced by ultraviolet light, cigarette smoke and pollution. The best natural sources of lutein are green and leafy vegetables, such as kale, spinach, chicory, celery and lettuce, green vegetables, orange-red tubers, fresh herbs and egg yolk.

18. Astaxanthin, a carotenoid belonging to the xanthophyll class, has aroused great interest due to its antioxidant capacity and possible role in reducing the risk of some diseases. Astaxanthin can be found naturally in microalgae such as Haematococcus pluvialis and in the yeast Phaffia rhodozyma as it has also been considered the main carotenoid in salmon and crustaceans. Shrimp processing residues, usually discarded, are also an important source of astaxanthin. The antioxidant activity of astaxanthin has demonstrated an important function in the modulation of biological functions related to lipid peroxidation, having beneficial effects in chronic diseases such as cardiovascular diseases, macular degeneration and cancer. Research has shown satisfactory effects of astaxanthin obtained from natural sources as well as that obtained synthetically, however studies in humans are limited to the use of natural sources.

19. Also called organic minerals, chelated minerals or chelated amino acid mineral. They are minerals linked to an amino acid and have a greater capacity to be absorbed by the body. They can be of three types: 1. Mineral Amino Acid Chelate: when a mineral molecule is linked to a specific amino acid. It is easily assimilated by the body. 2. Mineral Complex Amino Acid: (specific and nonspecific) when a mineral molecule is linked to a complex amino acid. It is less absorbed than the previous one. 3. Mineral Proteinate: when a mineral molecule is linked to a polypeptide complex. It is the least absorbed of the three types: The difference between the three types is in the molecular weight, the constant stability of bonds and the amino acids used. Chelated minerals have the advantage of being better bioavailable (up to 90% absorption, against 10 to 20% of inorganic minerals), without interfering with the absorption of other nutrients, without having side effects, or causing doppig. For calculating the correction of chelated minerals, medical prescription must be taken into account. If the request is only the pure mineral, which we call elementary content, the factor must be applied. If the prescription is chelated, no. To be sure at the time of prescription, the ideal is to evaluate by the prescribed dosage, so we know if the elementary is prescribed or not. Selenium offers protection against several cancers and, in fact, against a wide spectrum of diseases such as: chronic diseases, such as arterosclerosis (coronary artery disease, cerebrovascular disease and peripheral vascular disease), cancer, degenerative joint disease (arthritis), cirrhosis and chronic obstructive pulmonary disease (emphysema).

20. Quercetin is an antioxidant flavonoid, which is present in food in the form of natural glycosides and can be found in vegetables, fruits and juices. Various therapeutic properties of flavonoids, especially Quercetin, have been studied in recent decades, highlighting the antioxidant, anticarcinogenic potential and their protective effects on the renal, cardiovascular and hepatic systems. It is also a powerful antioxidant and free anti-radicals, reducing the risk of death from coronary heart disease and decreasing the incidence of myocardial infarction. Features- in the form of a yellow-gold powder.

21. Bromelain is a digestive enzyme of plant origin - Ananas comosus with anti-inflammatory action. In addition to its anti-inflammatory action, its efficiency in inhibiting the development of cancer cells has been studied. Recommendation for use Low Dosages: 50 to 100 mg / day, Larger Dosages: 500 mg / day Used in inflammatory processes of traumatic origin, infectious, vascular and rheumatic surgery. Properties Digestive enzyme, it has an anti-inflammatory action produced by the fibrinolytic and anti-fibriniquinic action of bromelains. Indications Used in inflammatory processes of traumatic origin, infectious surgery, vascular and rheumatic. Bromelain can also be used as an aid in digestion and for the treatment of high-grade burns.

22. Vitamin C, ascorbic acid, participates in several biochemical actions vital to the body. It improves the immune system, the skin, the mood and prevents eye problems and strokes. The nutrient also has a strong antioxidant action, fighting free radicals.

23. Improves immunity: Vitamin C increases the production of white blood cells, cells that are part of the immune system and that have the function of fighting microorganisms and foreign structures in the body. The nutrient also increases the levels of antibodies in the body. Thus, the nutrient helps to strengthen the immune system, making our body less susceptible to disease.

24 _. Prevents skin aging: Vitamin C prevents skin aging as it is essential for the natural production of collagen by the body. Collagen is a protein that provides support and firmness to the skin. In addition, vitamin C has an antioxidant action, that is, it neutralizes free radicals, protecting the skin against collagen degradation.

25. Improves iron absorption: Vitamin C increases the bioavailability of non-heme iron, that of plant origin, in the body.

26. Provides resistance to bones: This is because vitamin C is necessary for the production of collagen. This protein is not only beneficial for the skin, but also provides resistance to bones, teeth, tendons and blood vessel walls.

27. Prevents vision problems: Vitamin C contributes to prevent vision problems due to aging. This is because the nutrient is one of the factors for the prevention of macula degeneration, part of the retina responsible for the perception of details. Other nutrients that prevent the problem are beta-carotene, vitamin E, zinc and copper.

28. Lipedema is a dysfunction of fat distribution, affecting almost exclusively women, whose tissues are structured differently from men. The predisposition for lipedema is likely to be genetic. The cause of this chronic disease is usually hormonal changes in the body, which happen during puberty, pregnancy or menopause. If the condition already exists, the symptoms are likely to worsen at these times in life. 29. Lipedema is characterized by an increase in subcutaneous adipose tissue (lipohypertrophy), swelling in the second half of the day and pain in the legs. The fat cells of the lipedema have a different constitution, e.g. the fat reserve in the belly.

30. Virtually only women are affected by lipedema. Therefore, experts assume that the main causes are hormonal. The disease usually manifests itself at the end of puberty or during pregnancy. In the few men diagnosed with lipedema, its origin is often due to hormonal changes.

31. Lipedema is not a fat reserve due to excessive weight, but rather a pathological change in adipose tissue. However, excessive weight and weight fluctuations have a negative effect on lipedema.

32. Unlike lymphedema, lipedema is symmetrical: it causes changes in the "spine" type and deformations of the legs. Hips, thighs and legs are typically bulky.

33. If the disease extends further down, Suaven trousers are spoken of, as the deformations usually end in the ankles, overlapped by fat. Lipedema fat is sensitive to pressure and touch pain. In advanced stages, even tighter clothing already causes pain. Unlike lymphedema, in lipedema Stemmer's sign is always negative.

Currently observed drawbacks:

34. In possible cases, liposuction operations are recommended, provided that there is then no fluctuation in weight or a sudden increase in weight. 35. Otherwise, there is a danger that fat folds will re-form after some time.

36. In principle, after liposuction pits can form in the skin, which can be largely avoided with the use of special compression stockings. Before liposuction, it is imperative to clarify whether the lymphatic system is already affected by the disease, as, in this case, it has to do without liposuction.

Solution:

37. Therefore, thinking about solving these inconveniences and offering a practical, safe and efficient solution, the drug in question was developed. Also presenting several benefits, which can be highlighted in:

• Drug treatment;

• Avoids general disorders;

• Reduces costs, as it avoids removal of professionals;

• Offers more practical treatment;

• Industrial feasibility;

• Innovations worthy of this patent privilege.

State of the art:

38. Currently, no drug and remedy treatment for “Lipedema” is known.

39. For a perfect visualization and understanding of the “ORAL MEDICATION TO TREAT LIPEDEMA”, in question, follow the illustrative drawings, where:

40. Fig. 1— It shows an illustrative view of legs with lipedema swelling in early to more advanced stages; 41. Fig. 2 - It shows an illustrative view of the arm with swelling of the lipedema;

42. Fig. 3 - Shows an illustrative view of the thighs with swelling of the lipedema;

43. Fig. 4 - It presents a view of the biosynthetic proposal scheme for the formation of piperine;

44. Fig. 5 - Displays a view of the chemical component curcumin scheme.

45. According to the illustration and in its details, the “ORAL MEDICATION TO TREAT LIPEDEMA is characterized by being a drug formulation for oral use for the treatment of lipedema (1) in humans (H) containing: dry melon extract cataloupe equivalent to 480UI super oxide dismutase (2), pyrroloquinoline quinone 5 mg (3), citrus sinensis 400 mg (4), curcumin 100 mg (5), piperine 2 mg (6), lutein 5 mg (7), astaxanthin 1 mg (8), selenium chelate 100 mcg (9), vitamin C 100 mg (10), quercetin 300mg (11) and bromelain 180mg (12).

46. Due to the advantages it offers and because it has truly innovative characteristics, the “ORAL MEDICATION TO TREAT LIPEDEMA”, brings together the necessary conditions to merit the Invention Patent.

Claims

1 ^a ) “ORAL MEDICATION TO TREAT UPEDEMA” is characterized by being constituted of an oral medication formula for the treatment of lipedema (1) in humans (H) containing; dry extract of melon cataloupe equivalent 480UI super oxide dismutase (2), pyrroloquinoline quinone 5 mg (3), citrus sinensis 400 mg (4), curcumin 100 mg (5), piperine 2 mg (6), lutein 5 mg (7) , astaxanthin 1 mg (8), selenium chelate 100 mcg (9), vitamin C 100 mg (10), quercetin 300 mg (11) and bromelain 180 mg (12).